SG181727A1 - Topical ophthalmic peptide formulation - Google Patents
Topical ophthalmic peptide formulation Download PDFInfo
- Publication number
- SG181727A1 SG181727A1 SG2012044178A SG2012044178A SG181727A1 SG 181727 A1 SG181727 A1 SG 181727A1 SG 2012044178 A SG2012044178 A SG 2012044178A SG 2012044178 A SG2012044178 A SG 2012044178A SG 181727 A1 SG181727 A1 SG 181727A1
- Authority
- SG
- Singapore
- Prior art keywords
- somatostatin
- ophthalmic composition
- eye
- topical ophthalmic
- composition according
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 40
- 230000000699 topical effect Effects 0.000 title claims abstract description 35
- 108090000765 processed proteins & peptides Proteins 0.000 title claims abstract description 19
- 238000009472 formulation Methods 0.000 title abstract description 9
- 238000011282 treatment Methods 0.000 claims abstract description 30
- 208000030533 eye disease Diseases 0.000 claims abstract description 17
- 230000002265 prevention Effects 0.000 claims abstract description 17
- NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical group C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 claims description 88
- 108010056088 Somatostatin Proteins 0.000 claims description 80
- 102000005157 Somatostatin Human genes 0.000 claims description 79
- 229960000553 somatostatin Drugs 0.000 claims description 57
- 239000003889 eye drop Substances 0.000 claims description 38
- 229940012356 eye drops Drugs 0.000 claims description 36
- 108010016076 Octreotide Proteins 0.000 claims description 25
- 229960002700 octreotide Drugs 0.000 claims description 25
- DEQANNDTNATYII-OULOTJBUSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 DEQANNDTNATYII-OULOTJBUSA-N 0.000 claims description 24
- 239000007864 aqueous solution Substances 0.000 claims description 14
- -1 somatostatin-13 Chemical compound 0.000 claims description 14
- 229940075620 somatostatin analogue Drugs 0.000 claims description 11
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 8
- 239000006196 drop Substances 0.000 claims description 8
- 239000002674 ointment Substances 0.000 claims description 8
- 108050001286 Somatostatin Receptor Proteins 0.000 claims description 7
- 102000011096 Somatostatin receptor Human genes 0.000 claims description 7
- SWXOGPJRIDTIRL-DOUNNPEJSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-n-[(2s)-1-amino-3-(1h-indol-3-yl)-1-oxopropan-2-yl]-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pent Chemical compound C([C@H]1C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](N)CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(N)=O)=O)C(C)C)C1=CC=C(O)C=C1 SWXOGPJRIDTIRL-DOUNNPEJSA-N 0.000 claims description 6
- 102100030851 Cortistatin Human genes 0.000 claims description 6
- 229930185483 Cortistatin Natural products 0.000 claims description 6
- 108010005430 cortistatin Proteins 0.000 claims description 6
- DDRPLNQJNRBRNY-WYYADCIBSA-N cortistatin-14 Chemical compound C([C@H]1C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N1)NC(=O)[C@H]1NCCC1)C(=O)N[C@@H](CCCCN)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 DDRPLNQJNRBRNY-WYYADCIBSA-N 0.000 claims description 6
- 229960002730 vapreotide Drugs 0.000 claims description 6
- 108700029852 vapreotide Proteins 0.000 claims description 6
- 102100029563 Somatostatin Human genes 0.000 claims description 5
- 101800004701 Somatostatin-28 Proteins 0.000 claims description 5
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 5
- GGYTXJNZMFRSLX-DFTNLTQTSA-N somatostatin-28 Chemical compound N([C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1C(N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CSSC1)C(O)=O)[C@@H](C)O)[C@@H](C)O)=O)C(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO GGYTXJNZMFRSLX-DFTNLTQTSA-N 0.000 claims description 5
- 208000001344 Macular Edema Diseases 0.000 claims description 4
- 208000017442 Retinal disease Diseases 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- NPJIOCBFOAHEDO-AVWFULIKSA-N (3s,6s,9s,12r,15s,18s)-9-(4-aminobutyl)-3-benzyl-15-[(4-hydroxyphenyl)methyl]-12-(1h-indol-3-ylmethyl)-1,18-dimethyl-6-propan-2-yl-1,4,7,10,13,16-hexazacyclooctadecane-2,5,8,11,14,17-hexone Chemical compound C([C@H]1C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N[C@@H](CC=2C=CC=CC=2)C(=O)N(C)[C@@H](C)C(=O)N1)=O)C(C)C)C1=CC=C(O)C=C1 NPJIOCBFOAHEDO-AVWFULIKSA-N 0.000 claims description 3
- PUDHBTGHUJUUFI-SCTWWAJVSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-n-[(2s,3r)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2r)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-p Chemical compound C([C@H]1C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](N)CC=1C=C2C=CC=CC2=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(N)=O)=O)C(C)C)C1=CC=C(O)C=C1 PUDHBTGHUJUUFI-SCTWWAJVSA-N 0.000 claims description 3
- 206010025415 Macular oedema Diseases 0.000 claims description 3
- 239000002202 Polyethylene glycol Chemical group 0.000 claims description 3
- 206010038923 Retinopathy Diseases 0.000 claims description 3
- 125000002252 acyl group Chemical group 0.000 claims description 3
- 206010064930 age-related macular degeneration Diseases 0.000 claims description 3
- 230000008901 benefit Effects 0.000 claims description 3
- 125000003827 glycol group Chemical group 0.000 claims description 3
- 108010021336 lanreotide Proteins 0.000 claims description 3
- 229960002437 lanreotide Drugs 0.000 claims description 3
- 208000002780 macular degeneration Diseases 0.000 claims description 3
- 201000010230 macular retinal edema Diseases 0.000 claims description 3
- 229960005415 pasireotide Drugs 0.000 claims description 3
- 108700017947 pasireotide Proteins 0.000 claims description 3
- VMZMNAABQBOLAK-DBILLSOUSA-N pasireotide Chemical compound C([C@H]1C(=O)N2C[C@@H](C[C@H]2C(=O)N[C@H](C(=O)N[C@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@H](C(N[C@@H](CC=2C=CC(OCC=3C=CC=CC=3)=CC=2)C(=O)N1)=O)CCCCN)C=1C=CC=CC=1)OC(=O)NCCN)C1=CC=CC=C1 VMZMNAABQBOLAK-DBILLSOUSA-N 0.000 claims description 3
- 230000035699 permeability Effects 0.000 claims description 3
- 229920001223 polyethylene glycol Chemical group 0.000 claims description 3
- 239000003755 preservative agent Substances 0.000 claims description 3
- GGYTXJNZMFRSLX-UHFFFAOYSA-N prosomatostatin Chemical compound C1CCC(C(=O)NC(CCCNC(N)=N)C(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NCC(=O)NC2C(NC(CCCCN)C(=O)NC(CC(N)=O)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C4=CC=CC=C4NC=3)C(=O)NC(CCCCN)C(=O)NC(C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(C(=O)NC(CO)C(=O)NC(CSSC2)C(O)=O)C(C)O)C(C)O)=O)N1C(=O)C(C)NC(=O)C(CCSC)NC(=O)C(C)NC(=O)C1CCCN1C(=O)C(CC(N)=O)NC(=O)C(CO)NC(=O)C(CC(N)=O)NC(=O)C(C)NC(=O)C(N)CO GGYTXJNZMFRSLX-UHFFFAOYSA-N 0.000 claims description 3
- 108010001670 prosomatostatin Proteins 0.000 claims description 3
- 229950002758 seglitide Drugs 0.000 claims description 3
- 108010052231 seglitide Proteins 0.000 claims description 3
- 208000005590 Choroidal Neovascularization Diseases 0.000 claims description 2
- 206010060823 Choroidal neovascularisation Diseases 0.000 claims description 2
- 208000007014 Retinitis pigmentosa Diseases 0.000 claims description 2
- 206010038933 Retinopathy of prematurity Diseases 0.000 claims description 2
- 206010038935 Retinopathy sickle cell Diseases 0.000 claims description 2
- 206010046851 Uveitis Diseases 0.000 claims description 2
- 201000007917 background diabetic retinopathy Diseases 0.000 claims description 2
- 208000028867 ischemia Diseases 0.000 claims description 2
- 230000002335 preservative effect Effects 0.000 claims description 2
- 201000007914 proliferative diabetic retinopathy Diseases 0.000 claims description 2
- 208000007135 Retinal Neovascularization Diseases 0.000 claims 1
- 210000001957 retinal vein Anatomy 0.000 claims 1
- 208000022873 Ocular disease Diseases 0.000 abstract description 2
- 102000004196 processed proteins & peptides Human genes 0.000 abstract description 2
- 210000001508 eye Anatomy 0.000 description 50
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 23
- 206010012601 diabetes mellitus Diseases 0.000 description 20
- 241000700159 Rattus Species 0.000 description 18
- 210000004027 cell Anatomy 0.000 description 16
- 239000000243 solution Substances 0.000 description 15
- 239000003814 drug Substances 0.000 description 13
- 239000008194 pharmaceutical composition Substances 0.000 description 12
- 210000001525 retina Anatomy 0.000 description 12
- 239000011780 sodium chloride Substances 0.000 description 12
- ZSJLQEPLLKMAKR-GKHCUFPYSA-N streptozocin Chemical compound O=NN(C)C(=O)N[C@H]1[C@@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O ZSJLQEPLLKMAKR-GKHCUFPYSA-N 0.000 description 12
- ZSJLQEPLLKMAKR-UHFFFAOYSA-N Streptozotocin Natural products O=NN(C)C(=O)NC1C(O)OC(CO)C(O)C1O ZSJLQEPLLKMAKR-UHFFFAOYSA-N 0.000 description 11
- 229960001052 streptozocin Drugs 0.000 description 11
- 241001465754 Metazoa Species 0.000 description 9
- 230000001954 sterilising effect Effects 0.000 description 9
- 230000001640 apoptogenic effect Effects 0.000 description 8
- 229940079593 drug Drugs 0.000 description 8
- 210000004127 vitreous body Anatomy 0.000 description 8
- 230000002207 retinal effect Effects 0.000 description 7
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 6
- 238000002347 injection Methods 0.000 description 6
- 239000007924 injection Substances 0.000 description 6
- 239000003981 vehicle Substances 0.000 description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 230000004914 glial activation Effects 0.000 description 5
- 238000002372 labelling Methods 0.000 description 5
- 239000002502 liposome Substances 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- 230000000007 visual effect Effects 0.000 description 5
- 241000283973 Oryctolagus cuniculus Species 0.000 description 4
- 201000007737 Retinal degeneration Diseases 0.000 description 4
- 238000000942 confocal micrograph Methods 0.000 description 4
- 230000002596 correlated effect Effects 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- 239000002088 nanocapsule Substances 0.000 description 4
- 230000004770 neurodegeneration Effects 0.000 description 4
- 229940068196 placebo Drugs 0.000 description 4
- 239000000902 placebo Substances 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- 230000004258 retinal degeneration Effects 0.000 description 4
- 210000002966 serum Anatomy 0.000 description 4
- 230000009885 systemic effect Effects 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- KBTLDMSFADPKFJ-UHFFFAOYSA-N 2-phenyl-1H-indole-3,4-dicarboximidamide Chemical compound N1C2=CC=CC(C(N)=N)=C2C(C(=N)N)=C1C1=CC=CC=C1 KBTLDMSFADPKFJ-UHFFFAOYSA-N 0.000 description 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- 208000003098 Ganglion Cysts Diseases 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 241000699670 Mus sp. Species 0.000 description 3
- 208000005400 Synovial Cyst Diseases 0.000 description 3
- 230000000875 corresponding effect Effects 0.000 description 3
- 238000002571 electroretinography Methods 0.000 description 3
- 230000014509 gene expression Effects 0.000 description 3
- 239000000693 micelle Substances 0.000 description 3
- 210000004940 nucleus Anatomy 0.000 description 3
- 230000003534 oscillatory effect Effects 0.000 description 3
- 239000011148 porous material Substances 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 108090000586 somatostatin receptor 2 Proteins 0.000 description 3
- 102000004052 somatostatin receptor 2 Human genes 0.000 description 3
- 238000007920 subcutaneous administration Methods 0.000 description 3
- 238000007910 systemic administration Methods 0.000 description 3
- 229940124597 therapeutic agent Drugs 0.000 description 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical class OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- CFKMVGJGLGKFKI-UHFFFAOYSA-N 4-chloro-m-cresol Chemical compound CC1=CC(O)=CC=C1Cl CFKMVGJGLGKFKI-UHFFFAOYSA-N 0.000 description 2
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 2
- 241000283707 Capra Species 0.000 description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 230000006907 apoptotic process Effects 0.000 description 2
- 229960000686 benzalkonium chloride Drugs 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 2
- 229940098773 bovine serum albumin Drugs 0.000 description 2
- 210000005252 bulbus oculi Anatomy 0.000 description 2
- OSASVXMJTNOKOY-UHFFFAOYSA-N chlorobutanol Chemical compound CC(C)(O)C(Cl)(Cl)Cl OSASVXMJTNOKOY-UHFFFAOYSA-N 0.000 description 2
- 210000003161 choroid Anatomy 0.000 description 2
- 238000013461 design Methods 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 239000003885 eye ointment Substances 0.000 description 2
- 229930195729 fatty acid Natural products 0.000 description 2
- 239000000194 fatty acid Substances 0.000 description 2
- 150000004665 fatty acids Chemical class 0.000 description 2
- 150000002195 fatty ethers Chemical class 0.000 description 2
- 230000007277 glial cell activation Effects 0.000 description 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 2
- 239000000017 hydrogel Substances 0.000 description 2
- 239000007943 implant Substances 0.000 description 2
- 238000007918 intramuscular administration Methods 0.000 description 2
- 150000002632 lipids Chemical class 0.000 description 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 2
- 239000007908 nanoemulsion Substances 0.000 description 2
- 239000002105 nanoparticle Substances 0.000 description 2
- 229940069265 ophthalmic ointment Drugs 0.000 description 2
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 description 2
- XJMOSONTPMZWPB-UHFFFAOYSA-M propidium iodide Chemical compound [I-].[I-].C12=CC(N)=CC=C2C2=CC=C(N)C=C2[N+](CCC[N+](C)(CC)CC)=C1C1=CC=CC=C1 XJMOSONTPMZWPB-UHFFFAOYSA-M 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 210000003583 retinal pigment epithelium Anatomy 0.000 description 2
- 239000000523 sample Substances 0.000 description 2
- 230000009291 secondary effect Effects 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 229940035636 somatostatin and analogues Drugs 0.000 description 2
- 238000010186 staining Methods 0.000 description 2
- 238000011477 surgical intervention Methods 0.000 description 2
- 238000011200 topical administration Methods 0.000 description 2
- 238000002604 ultrasonography Methods 0.000 description 2
- 238000001262 western blot Methods 0.000 description 2
- WPRAXAOJIODQJR-UHFFFAOYSA-N 1-(3,4-dimethylphenyl)ethanone Chemical compound CC(=O)C1=CC=C(C)C(C)=C1 WPRAXAOJIODQJR-UHFFFAOYSA-N 0.000 description 1
- JKXYOQDLERSFPT-UHFFFAOYSA-N 2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(2-octadecoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol Chemical compound CCCCCCCCCCCCCCCCCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO JKXYOQDLERSFPT-UHFFFAOYSA-N 0.000 description 1
- HBTAOSGHCXUEKI-UHFFFAOYSA-N 4-chloro-n,n-dimethyl-3-nitrobenzenesulfonamide Chemical compound CN(C)S(=O)(=O)C1=CC=C(Cl)C([N+]([O-])=O)=C1 HBTAOSGHCXUEKI-UHFFFAOYSA-N 0.000 description 1
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical class OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 239000012099 Alexa Fluor family Substances 0.000 description 1
- 241000837181 Andina Species 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- 201000004569 Blindness Diseases 0.000 description 1
- 108010017384 Blood Proteins Proteins 0.000 description 1
- 102000004506 Blood Proteins Human genes 0.000 description 1
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 description 1
- 238000011740 C57BL/6 mouse Methods 0.000 description 1
- 208000002177 Cataract Diseases 0.000 description 1
- 241000718430 Comocladia glabra Species 0.000 description 1
- 206010058202 Cystoid macular oedema Diseases 0.000 description 1
- 108010008286 DNA nucleotidylexotransferase Proteins 0.000 description 1
- 102100029764 DNA-directed DNA/RNA polymerase mu Human genes 0.000 description 1
- AHCYMLUZIRLXAA-SHYZEUOFSA-N Deoxyuridine 5'-triphosphate Chemical compound O1[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)[C@@H](O)C[C@@H]1N1C(=O)NC(=O)C=C1 AHCYMLUZIRLXAA-SHYZEUOFSA-N 0.000 description 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical class OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 1
- 108010041308 Endothelial Growth Factors Proteins 0.000 description 1
- 101000888419 Homo sapiens Glial fibrillary acidic protein Proteins 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 206010025421 Macule Diseases 0.000 description 1
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 description 1
- 206010038848 Retinal detachment Diseases 0.000 description 1
- 241001168730 Simo Species 0.000 description 1
- 229920004890 Triton X-100 Polymers 0.000 description 1
- 239000013504 Triton X-100 Substances 0.000 description 1
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 description 1
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 description 1
- 229930003427 Vitamin E Chemical class 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000001464 adherent effect Effects 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 239000000048 adrenergic agonist Substances 0.000 description 1
- 239000000674 adrenergic antagonist Substances 0.000 description 1
- 125000005907 alkyl ester group Chemical group 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 230000003444 anaesthetic effect Effects 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000004037 angiogenesis inhibitor Substances 0.000 description 1
- 230000000340 anti-metabolite Effects 0.000 description 1
- 230000002137 anti-vascular effect Effects 0.000 description 1
- 239000000427 antigen Substances 0.000 description 1
- 102000036639 antigens Human genes 0.000 description 1
- 108091007433 antigens Proteins 0.000 description 1
- 229940006133 antiglaucoma drug and miotics carbonic anhydrase inhibitors Drugs 0.000 description 1
- 239000002256 antimetabolite Substances 0.000 description 1
- 229940100197 antimetabolite Drugs 0.000 description 1
- 210000000026 apposition eye Anatomy 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- 102000012740 beta Adrenergic Receptors Human genes 0.000 description 1
- 108010079452 beta Adrenergic Receptors Proteins 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 1
- 239000004327 boric acid Substances 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000003489 carbonate dehydratase inhibitor Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 210000003855 cell nucleus Anatomy 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 229960004926 chlorobutanol Drugs 0.000 description 1
- 229960002242 chlorocresol Drugs 0.000 description 1
- 210000004240 ciliary body Anatomy 0.000 description 1
- 238000004624 confocal microscopy Methods 0.000 description 1
- 210000000795 conjunctiva Anatomy 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 210000004087 cornea Anatomy 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 229960001334 corticosteroids Drugs 0.000 description 1
- 229940124570 cycloplegic agent Drugs 0.000 description 1
- 230000003500 cycloplegic effect Effects 0.000 description 1
- 201000010206 cystoid macular edema Diseases 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 125000003074 decanoyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C(*)=O 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 238000010217 densitometric analysis Methods 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- SOROIESOUPGGFO-UHFFFAOYSA-N diazolidinylurea Chemical compound OCNC(=O)N(CO)C1N(CO)C(=O)N(CO)C1=O SOROIESOUPGGFO-UHFFFAOYSA-N 0.000 description 1
- 229960001083 diazolidinylurea Drugs 0.000 description 1
- 229940031578 diisopropyl adipate Drugs 0.000 description 1
- 239000004205 dimethyl polysiloxane Substances 0.000 description 1
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 1
- 230000008034 disappearance Effects 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 206010014801 endophthalmitis Diseases 0.000 description 1
- 210000000981 epithelium Anatomy 0.000 description 1
- 210000000744 eyelid Anatomy 0.000 description 1
- 230000004438 eyesight Effects 0.000 description 1
- 150000002191 fatty alcohols Chemical class 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Chemical class CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 230000002518 glial effect Effects 0.000 description 1
- 239000003862 glucocorticoid Substances 0.000 description 1
- 150000002398 hexadecan-1-ols Chemical class 0.000 description 1
- 125000003104 hexanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 102000051520 human GFAP Human genes 0.000 description 1
- 238000003364 immunohistochemistry Methods 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 230000004410 intraocular pressure Effects 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 239000000644 isotonic solution Substances 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 210000004561 lacrimal apparatus Anatomy 0.000 description 1
- 125000000400 lauroyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002669 linoleoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])/C([H])=C([H])\C([H])([H])/C([H])=C([H])\C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 239000006193 liquid solution Substances 0.000 description 1
- QSHDDOUJBYECFT-UHFFFAOYSA-N mercury Chemical compound [Hg] QSHDDOUJBYECFT-UHFFFAOYSA-N 0.000 description 1
- 229910052753 mercury Inorganic materials 0.000 description 1
- 108020004999 messenger RNA Proteins 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000003604 miotic agent Substances 0.000 description 1
- 125000001419 myristoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000002077 nanosphere Substances 0.000 description 1
- 239000002353 niosome Substances 0.000 description 1
- 125000002801 octanoyl group Chemical group C(CCCCCCC)(=O)* 0.000 description 1
- 125000002811 oleoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])/C([H])=C([H])\C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 210000001328 optic nerve Anatomy 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 150000002902 organometallic compounds Chemical class 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 244000052769 pathogen Species 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 1
- 239000004417 polycarbonate Substances 0.000 description 1
- 229920000515 polycarbonate Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- 150000004040 pyrrolidinones Chemical class 0.000 description 1
- 230000004264 retinal detachment Effects 0.000 description 1
- 230000004243 retinal function Effects 0.000 description 1
- 208000004644 retinal vein occlusion Diseases 0.000 description 1
- 238000004007 reversed phase HPLC Methods 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical class OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 1
- 229930182490 saponin Natural products 0.000 description 1
- 150000007949 saponins Chemical class 0.000 description 1
- 235000017709 saponins Nutrition 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 108010082379 somatostatin receptor type 1 Proteins 0.000 description 1
- 238000012453 sprague-dawley rat model Methods 0.000 description 1
- 125000003696 stearoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 238000000108 ultra-filtration Methods 0.000 description 1
- 230000004304 visual acuity Effects 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 239000011709 vitamin E Chemical class 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000003871 white petrolatum Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/31—Somatostatins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Liposomes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/51—Nanocapsules; Nanoparticles
- A61K9/5107—Excipients; Inactive ingredients
- A61K9/513—Organic macromolecular compounds; Dendrimers
- A61K9/5146—Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
- A61K9/5153—Polyesters, e.g. poly(lactide-co-glycolide)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
- Dispersion Chemistry (AREA)
- Biomedical Technology (AREA)
- Optics & Photonics (AREA)
- Nanotechnology (AREA)
- Physics & Mathematics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES200931242A ES2362604B1 (es) | 2009-12-22 | 2009-12-22 | Formulación tópica oftálmica de péptidos. |
| PCT/EP2010/007737 WO2011076368A2 (en) | 2009-12-22 | 2010-12-17 | Topical ophthalmic peptide formulation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG181727A1 true SG181727A1 (en) | 2012-07-30 |
Family
ID=43928893
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG2012044178A SG181727A1 (en) | 2009-12-22 | 2010-12-17 | Topical ophthalmic peptide formulation |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US9216208B2 (ko) |
| EP (1) | EP2515870B1 (ko) |
| JP (1) | JP5920928B2 (ko) |
| KR (1) | KR101657737B1 (ko) |
| CN (1) | CN102753153B (ko) |
| AR (1) | AR079683A1 (ko) |
| AU (1) | AU2010335595B2 (ko) |
| BR (1) | BR112012015386B8 (ko) |
| CA (1) | CA2785104C (ko) |
| CL (1) | CL2012001737A1 (ko) |
| CO (1) | CO6592047A2 (ko) |
| CY (1) | CY1117854T1 (ko) |
| DK (1) | DK2515870T3 (ko) |
| ES (2) | ES2362604B1 (ko) |
| HK (1) | HK1178049A1 (ko) |
| HR (1) | HRP20160954T1 (ko) |
| HU (1) | HUE028193T2 (ko) |
| IL (1) | IL220584A (ko) |
| LT (1) | LT2515870T (ko) |
| MX (1) | MX338323B (ko) |
| MY (1) | MY178169A (ko) |
| NZ (1) | NZ600627A (ko) |
| PL (1) | PL2515870T3 (ko) |
| PT (1) | PT2515870T (ko) |
| RS (1) | RS54953B1 (ko) |
| RU (1) | RU2561585C2 (ko) |
| SG (1) | SG181727A1 (ko) |
| SI (1) | SI2515870T1 (ko) |
| SM (1) | SMT201600277B (ko) |
| TW (1) | TWI548416B (ko) |
| UA (1) | UA108484C2 (ko) |
| UY (1) | UY33153A (ko) |
| WO (1) | WO2011076368A2 (ko) |
| ZA (1) | ZA201204522B (ko) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2968471B1 (en) | 2013-03-01 | 2017-07-19 | Fundació Hospital Universitari Vall d' Hebron - Institut de Recerca | Peptides for use in the topical treatment of retinal neurodegenerative diseases, in particular in early stages of diabetic retinopathy and other retinal diseases in which neurodegeneration plays an essential role |
| GB201516066D0 (en) * | 2015-09-10 | 2015-10-28 | Young & Co Llp D | Treatment of retinitis pigmentosa |
| CN106822182A (zh) * | 2016-12-27 | 2017-06-13 | 广州姿生生物科技有限公司 | 一种细胞提取物及其用途 |
| US11252960B2 (en) | 2017-01-31 | 2022-02-22 | Kimberly-Clark Worldwide, Inc. | Antibacterial composition including benzoic acid ester and methods of inhibiting bacterial growth utilizing the same |
| US20180325993A1 (en) | 2017-05-15 | 2018-11-15 | Sun Pharmaceutical Industries Limited | Octreotide injection |
| US20230025836A1 (en) * | 2019-11-21 | 2023-01-26 | Samjin Pharmaceutical Co., Ltd. | Eye drop composition for preventing or treating eye disease |
| KR20230133595A (ko) * | 2022-03-11 | 2023-09-19 | 한국한의약진흥원 | 등검은말벌독에 함유된 세로토닌의 안정성을 유지하기 위한 조성물 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5182258A (en) | 1989-03-20 | 1993-01-26 | Orbon Corporation | Systemic delivery of polypeptides through the eye |
| AU1307399A (en) * | 1997-11-06 | 1999-05-31 | Orbon Corporation | Stabilized, dry pharmaceutical compositions for drug delivery and methods of preparing same |
| CA2263042A1 (en) * | 1999-02-25 | 2000-08-25 | Robert W.A. Kuijpers | Treatment of edema |
| EP1040837A3 (en) * | 1999-02-26 | 2002-01-02 | Erasmus Universiteit Rotterdam | Medicaments for the treatment of a choroidal neovascularization (CNV) related disorder |
| AU2001283957A1 (en) | 2000-07-27 | 2002-02-13 | Novartis Ag | Treatment of ocular disorders with somatostatin analogues |
| TWI260228B (en) * | 2002-12-31 | 2006-08-21 | Ind Tech Res Inst | Delivery carrier of presenting cell of somatostatin receptor |
| US20050074497A1 (en) | 2003-04-09 | 2005-04-07 | Schultz Clyde L. | Hydrogels used to deliver medicaments to the eye for the treatment of posterior segment diseases |
| US8871269B2 (en) | 2003-07-15 | 2014-10-28 | Evonik Corporation | Method for the preparation of controlled release formulations |
| WO2007038687A2 (en) * | 2005-09-27 | 2007-04-05 | Aciont, Inc. | Ocular administration of immunosuppressive agents |
| CA2698833A1 (en) * | 2007-09-11 | 2009-03-19 | Mondobiotech Laboratories Ag | Use of a peptide as a therapeutic agent |
| ES2528409T3 (es) * | 2007-10-24 | 2015-02-10 | Camurus Ab | Formulaciones de liberación controlada |
-
2009
- 2009-12-22 ES ES200931242A patent/ES2362604B1/es not_active Expired - Fee Related
-
2010
- 2010-12-17 NZ NZ600627A patent/NZ600627A/en unknown
- 2010-12-17 RS RS20160598A patent/RS54953B1/sr unknown
- 2010-12-17 WO PCT/EP2010/007737 patent/WO2011076368A2/en active Application Filing
- 2010-12-17 CN CN201080063430.8A patent/CN102753153B/zh active Active
- 2010-12-17 RU RU2012126028/15A patent/RU2561585C2/ru active
- 2010-12-17 EP EP10810911.7A patent/EP2515870B1/en active Active
- 2010-12-17 AU AU2010335595A patent/AU2010335595B2/en active Active
- 2010-12-17 SG SG2012044178A patent/SG181727A1/en unknown
- 2010-12-17 US US13/518,617 patent/US9216208B2/en active Active
- 2010-12-17 BR BR112012015386A patent/BR112012015386B8/pt active IP Right Grant
- 2010-12-17 LT LTEP10810911.7T patent/LT2515870T/lt unknown
- 2010-12-17 ES ES10810911.7T patent/ES2587828T3/es active Active
- 2010-12-17 CA CA2785104A patent/CA2785104C/en active Active
- 2010-12-17 PT PT108109117T patent/PT2515870T/pt unknown
- 2010-12-17 UA UAA201207318A patent/UA108484C2/ru unknown
- 2010-12-17 DK DK10810911.7T patent/DK2515870T3/en active
- 2010-12-17 MY MYPI2012002758A patent/MY178169A/en unknown
- 2010-12-17 HU HUE10810911A patent/HUE028193T2/en unknown
- 2010-12-17 MX MX2012007282A patent/MX338323B/es active IP Right Grant
- 2010-12-17 PL PL10810911.7T patent/PL2515870T3/pl unknown
- 2010-12-17 JP JP2012545144A patent/JP5920928B2/ja active Active
- 2010-12-17 SI SI201031249A patent/SI2515870T1/sl unknown
- 2010-12-17 KR KR1020127019503A patent/KR101657737B1/ko active IP Right Grant
- 2010-12-21 AR ARP100104857A patent/AR079683A1/es not_active Application Discontinuation
- 2010-12-22 TW TW099145240A patent/TWI548416B/zh active
- 2010-12-22 UY UY0001033153A patent/UY33153A/es unknown
-
2012
- 2012-06-19 ZA ZA2012/04522A patent/ZA201204522B/en unknown
- 2012-06-21 IL IL220584A patent/IL220584A/en active IP Right Grant
- 2012-06-22 CL CL2012001737A patent/CL2012001737A1/es unknown
- 2012-07-10 CO CO12115592A patent/CO6592047A2/es unknown
-
2013
- 2013-04-26 HK HK13105067.2A patent/HK1178049A1/zh unknown
-
2016
- 2016-07-22 CY CY20161100721T patent/CY1117854T1/el unknown
- 2016-07-27 HR HRP20160954TT patent/HRP20160954T1/hr unknown
- 2016-08-16 SM SM201600277T patent/SMT201600277B/it unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2785104C (en) | Topical ophthalmic peptide formulation | |
| Tahara et al. | Feasibility of drug delivery to the eye's posterior segment by topical instillation of PLGA nanoparticles | |
| US11129900B2 (en) | Cytophilic peptide-fused high-density lipoprotein, and delivery of drug to posterior segment of eye by ocular installation of said fusion | |
| Soni et al. | Design and evaluation of ophthalmic delivery formulations | |
| Daull et al. | A preliminary evaluation of dexamethasone palmitate emulsion: a novel intravitreal sustained delivery of corticosteroid for treatment of macular edema | |
| Sarkar et al. | Nanodiagnostics and Nanotherapeutics for age-related macular degeneration | |
| Alvarez-Trabado et al. | Sorbitan ester nanoparticles (SENS) as a novel topical ocular drug delivery system: Design, optimization, and in vitro/ex vivo evaluation | |
| AU2017313907B2 (en) | Delivery of urea to cells of the macula and retina using liposome constructs | |
| Halasz et al. | Micro/nanoparticle delivery systems for ocular diseases | |
| Abla et al. | Lipid-based nanocarriers challenging the ocular biological barriers: Current paradigm and future perspectives | |
| Al-Amin et al. | Tailoring surface properties of liposomes for dexamethasone intraocular administration | |
| Sun et al. | Topical Ophthalmic Liposomes Dual-Modified with Penetratin and Hyaluronic Acid for the Noninvasive Treatment of Neovascular Age-Related Macular Degeneration | |
| Mori et al. | Potential of TAK-593 ophthalmic emulsion for the treatment of age-related macular degeneration | |
| Tavakoli | Intravitreal liposomes as ocular drug delivery systems: vitreal interactions, retinal permeation and drug release characteristics | |
| Badr | Topical Ocular Delivery to Posterior Eye Tissues | |
| Chaw | Fundamental study of nanoliposomes for ocular therapy | |
| Patel | Development and Evaluation of a Nanomicellar Eye Drop Formulation of Dexamethasone for Posterior Uveitis | |
| JP2020114809A (ja) | 黄斑浮腫抑制剤 | |
| CN115869416A (zh) | 用于眼部靶向递药的细胞膜、药物载体、组合物及其制备方法和用途 | |
| WO2023194797A1 (en) | Methods for treating eye diseases using lipid binding protein-based complexes | |
| Chowdhury | Development and preliminary in vitro evaluation of nanomicelles laden in situ gel of dexamethasone for ophthalmic delivery |